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Selective delivery of adapalene to the human hair follicle under finite dose conditions using polymeric micelle nanocarriers†
Nanoscale ( IF 5.8 ) Pub Date : 2017-12-18 00:00:00 , DOI: 10.1039/c7nr07706h Somnath G. Kandekar 1, 2, 3, 4 , Sergio del Río-Sancho 1, 2, 3, 4 , Maria Lapteva 1, 2, 3, 4 , Yogeshvar N. Kalia 1, 2, 3, 4
Nanoscale ( IF 5.8 ) Pub Date : 2017-12-18 00:00:00 , DOI: 10.1039/c7nr07706h Somnath G. Kandekar 1, 2, 3, 4 , Sergio del Río-Sancho 1, 2, 3, 4 , Maria Lapteva 1, 2, 3, 4 , Yogeshvar N. Kalia 1, 2, 3, 4
Affiliation
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Drug delivery systems that target the pilosebaceous unit (PSU) selectively could improve the clinical management of diseases that originate in the hair follicle. The aims of this study were (i) to prepare polymeric micelles using D-α-tocopheryl polyethylene glycol succinate diblock copolymer that incorporated adapalene (ADA), a retinoid indicated for Acne vulgaris, and (ii) to investigate the feasibility of delivering ADA preferentially to the PSU under finite dose conditions – thereby better approximating actual conditions of use by patients. Incorporation of ADA into spherical micelles (dn <20 nm) increased aqueous solubility by ∼50 000-fold (from <4 ng mL−1 to 0.2 mg mL−1). Optimized micelle solution and gel formulations (0.02% ADA) were stable after storage for 4 weeks at 4 °C. Finite dose experiments using full-thickness porcine and human skin revealed that ADA delivery efficiency from micelle solution and gel formulations was equivalent and was >2- and 10-fold higher than that from Differin® gel and Differin® cream (products containing ADA at 0.1% (w/w)). Follicular delivery studies in human skin, using a punch biopsy technique to extract the intact PSU, demonstrated that the micelle solution and gel formulations did indeed enable preferential delivery of ADA to the PSU (4.5- and 3.3-fold higher, respectively, than that to PSU-free skin biopsies). Confocal laser scanning microscopy provided visual corroboration that ADA was uniformly distributed in the hair follicles. In conclusion, the results confirmed that polymeric micelle nanocarriers enabled selective, targeted drug delivery to the PSU under finite dose conditions and so might improve therapy of follicular diseases and decrease off-site side-effects.
中文翻译：
使用聚合物胶束纳米载体在有限剂量条件下将阿达帕林选择性递送至人的毛囊†
选择性针对毛囊皮脂单位（PSU）的药物输送系统可以改善源自毛囊的疾病的临床管理。这项研究的目的是（i）使用掺入阿达帕林（ADA）的D -α-生育酚基聚乙二醇琥珀酸酯二嵌段共聚物制备聚合物胶束，该类化合物是寻常痤疮的一种类维生素A ，以及（ii）研究优先递送ADA的可行性在有限的剂量条件下使用PSU –从而更好地逼近患者的实际使用条件。将ADA掺入球形胶束（d n <20 nm）中可使水溶解度增加约50,000倍（从<4 ng mL -1到0.2 mg mL -1）。优化的胶束溶液和凝胶制剂（0.02％ADA）在4°C下储存4周后稳定。使用全厚度猪和人皮肤的有限剂量实验表明，胶束溶液和凝胶制剂的ADA传递效率相当，分别比Differin®凝胶和Differin®乳膏（含ADA的产品0.1倍）高2倍和10倍。 ％（w / w））。使用穿孔活检技术提取完整的PSU在人皮肤中进行的卵泡输送研究表明，胶束溶液和凝胶制剂确实能够使ADA优先输送到PSU（分别比PSU高4.5倍和3.3倍）。无PSU的皮肤活检）。共聚焦激光扫描显微镜提供了视觉证实，即ADA在毛囊中均匀分布。综上所述，
更新日期：2017-12-18
中文翻译：
使用聚合物胶束纳米载体在有限剂量条件下将阿达帕林选择性递送至人的毛囊†
选择性针对毛囊皮脂单位（PSU）的药物输送系统可以改善源自毛囊的疾病的临床管理。这项研究的目的是（i）使用掺入阿达帕林（ADA）的D -α-生育酚基聚乙二醇琥珀酸酯二嵌段共聚物制备聚合物胶束，该类化合物是寻常痤疮的一种类维生素A ，以及（ii）研究优先递送ADA的可行性在有限的剂量条件下使用PSU –从而更好地逼近患者的实际使用条件。将ADA掺入球形胶束（d n <20 nm）中可使水溶解度增加约50,000倍（从<4 ng mL -1到0.2 mg mL -1）。优化的胶束溶液和凝胶制剂（0.02％ADA）在4°C下储存4周后稳定。使用全厚度猪和人皮肤的有限剂量实验表明，胶束溶液和凝胶制剂的ADA传递效率相当，分别比Differin®凝胶和Differin®乳膏（含ADA的产品0.1倍）高2倍和10倍。 ％（w / w））。使用穿孔活检技术提取完整的PSU在人皮肤中进行的卵泡输送研究表明，胶束溶液和凝胶制剂确实能够使ADA优先输送到PSU（分别比PSU高4.5倍和3.3倍）。无PSU的皮肤活检）。共聚焦激光扫描显微镜提供了视觉证实，即ADA在毛囊中均匀分布。综上所述，
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